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European Journal of Drug Metabolism and Pharmacokinetics

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https://www.readbyqxmd.com/read/28283988/nicotine-population-pharmacokinetics-in-healthy-adult-smokers-a-retrospective-analysis
#1
Mathilde Marchand, Patrick Brossard, Henri Merdjan, Nicola Lama, Rolf Weitkunat, Frank Lüdicke
BACKGROUND AND OBJECTIVE: Characterizing nicotine pharmacokinetics is challenging in the presence of background exposure. We performed a combined retrospective population pharmacokinetic analysis of 8 trials, including exposure to Tobacco Heating System and cigarettes (both inhaled), nicotine nasal spray and oral nicotine gum. METHOD: Data from 4 single product use trials were used to develop a population pharmacokinetic model with Phoenix(®) NLME™ and to derive exposure parameters...
March 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28283987/evaluating-the-feasibility-of-use-of-a-foreign-reference-product-for-generic-drug-applications-a-retrospective-pilot-study
#2
Yi-Lin Wang, Li-Feng Hsu
BACKGROUND AND OBJECTIVES: The adoption of a domestic reference product in bioequivalence (BE) studies for generic drug applications is required by some countries. The objective of this study is to assess the feasibility of this by investigating whether innovative products from different countries are bioequivalent. METHODS: Data were collected from all generic drug applications received by the Taiwan regulatory authority 2012-2016. If a submission package contained BE studies, that generic product was compared separately with different reference products, and the resulting data included in this analysis...
March 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28276004/hydroxylation-metabolisms-of-crassicauline-a-in-rats-under-toxic-dose
#3
Xue Fan, Shan-Shan Yin, Xue-Jing Li, Kui Yang, Liang Xu, Ke Lan
BACKGROUND AND OBJECTIVES: Crassicauline A, a C19 diterpenoid alkaloid in Aconitum herbs, is an analgesic drug clinically used in China. The in vivo metabolism of crassicauline A is poorly understood, while potential bioactivation is anticipated via hydroxylation metabolism. This work, therefore, aimed to investigate the in vivo hydroxylation metabolism of crassicauline A in rats. METHODS: Using a de novo developed and validated UPLC-MS/MS method, excretion studies in rats were carried out to investigate the recoveries of crassicauline A and its hydroxylated metabolites in urine and feces...
March 8, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28260174/effect-of-gevokizumab-on-interleukin-1%C3%AE-mediated-cytochrome-p450-3a4-and-drug-transporter-repression-in-cultured-human-hepatocytes
#4
Amélie Moreau, Marc Le Vée, Elodie Jouan, Claire Denizot, Yannick Parmentier, Olivier Fardel
BACKGROUND AND OBJECTIVES: Gevokizumab is a potent anti-interleukin (IL)-1β neutralizing monoclonal antibody (mAb), which may be used for treating inflammatory or autoimmune diseases. The present study was designed to characterize the potential effects of this mAb towards well-established IL-1β-mediated repression of hepatic drug detoxifying proteins, like cytochrome P450 (CYP) 3A4 and drug transporters. METHODS: Primary cultured human hepatocytes were exposed to various concentrations of IL-1β in the absence or presence of gevokizumab (5 µg/mL); mRNA expression and activity of CYP3A4 and transporters were next determined...
March 4, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28255865/antioxidative-and-protective-actions-of-apigenin-in-a-paracetamol-induced-hepatotoxicity-rat-model
#5
Aleksandar Rašković, Slobodan Gigov, Ivan Čapo, Milica Paut Kusturica, Boris Milijašević, Sunčica Kojić-Damjanov, Nikola Martić
BACKGROUND AND OBJECTIVES: Apigenin is known to have various pharmacological properties without causing significant toxicity; however, hepatoprotective effect of apigenin is not often reported. The aim of our study was to investigate if the alterations in lipid peroxidation and antioxidant status are in favor to prove the efficacy of apigenin against paracetamol-induced hepatotoxicity. METHODS: The effect of apigenin on paracetamol-induced hepatotoxicity in rats was examined by determining biochemical parameters, histological assessment and oxidative status in liver homogenates...
March 2, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28236116/clinical-pharmacokinetic-and-pharmacodynamic-profile-of-lenvatinib-an-orally-active-small-molecule-multitargeted-tyrosine-kinase-inhibitor
#6
Ziad Hussein, Hitoshi Mizuo, Seiichi Hayato, Masayuki Namiki, Robert Shumaker
Lenvatinib is a multikinase inhibitor that targets vascular endothelial growth factor (VEGF) receptors 1-3, fibroblast growth factor receptors 1-4, platelet-derived growth factor receptor-alpha, and RET and KIT proto-oncogenes. Lenvatinib is approved for the treatment of radioiodine-refractory differentiated thyroid cancer in the United States (US), European Union (EU), Canada, Japan, and Switzerland. It is also approved in combination with everolimus for the treatment of advanced renal cell carcinoma following ≥1 VEGF-targeted treatment in the US and EU...
February 24, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28229434/preclinical-pharmacokinetics-and-pharmacodynamics-of-pinometostat-epz-5676-a-first-in-class-small-molecule-s-adenosyl-methionine-competitive-inhibitor-of-dot1l
#7
Nigel J Waters
Acute leukemias bearing mixed lineage leukemia (MLL) rearrangements are aggressive diseases characterized by a poor overall prognosis despite multi-agent chemotherapy. Aberrant fusion proteins involving the MLL histone methyltransferase (HMT) lead to recruitment of DOT1L, to a multi-protein complex resulting in aberrant methylation of histone H3 lysine 79 at MLL target genes, and ultimately enhanced expression of critical genes for hematopoietic differentiation, including HOXA9 and MEIS1, and as such defines the established mechanism for leukemogenesis in MLL-rearrangement (MLL-r) leukemias...
February 22, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28194579/prediction-of-tissue-to-plasma-ratios-of-basic-compounds-in-mice
#8
Prashant B Nigade, Jayasagar Gundu, K Sreedhara Pai, Kumar V S Nemmani
BACKGROUND: Majority of reported studies so far developed correlation regression equations using the rat muscle-to-plasma drug concentration ratio (Kp-muscle) to predict tissue-to-plasma drug concentration ratios (Kp-tissues). Use of regression equations derived from rat Kp-muscle may not be ideal to predict the mice tissue-Kps as there are species differences. OBJECTIVES: (i) To develop the linear regression equations using mouse tissue-Kps; (ii) to assess the correlation between organ blood flow and/or organ weight with tissue-Kps and (iii) compare the observed tissue-Kps from mice with corresponding predicted tissue-Kps using Richter's rat-Kp specific equations...
February 13, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28185143/characterization-of-1-aminobenzotriazole-and-ketoconazole-as-novel-inhibitors-of-monoamine-oxidase-mao-an-in-vitro-investigation
#9
Abdul Naveed Shaik, Barbara W LeDuc, Ansar A Khan
BACKGROUND AND OBJECTIVES: 1-Aminobenzotriazole, a known time-dependent inhibitor of cytochrome P450 (CYP) enzymes, and ketoconazole, a strong inhibitor of the human CYP3A4 isozyme, are used as standard probe inhibitors to characterize the CYP and/or non-CYP-mediated metabolism of xenobiotics. In the present investigation, 1-Aminobenzotriazole and ketoconazole are characterized as potent monoamine oxidase (MAO) inhibitors in vitro using mouse, rat and human liver microsomes and S9 fractions...
February 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28116646/systemic-bioavailability-and-dose-proportionality-of-omega-3-administered-in-free-fatty-acid-form-compared-with-ethyl-ester-form-results-of-a-phase-1-study-in-healthy-volunteers
#10
Elliot Offman, Michael Davidson, Mohammad Abu-Rashid, Peng Chai, Catarina Nilsson
BACKGROUND: Omega-3 carboxylic acids (OM3-CA) contains eicosapentaenoic acid (EPA) and docosahexaenoic acid (DHA) in free fatty acid form. Per gram, OM3-CA includes approximately half as much EPA as icosapent ethyl (IPE), an ethyl ester formulation of EPA. OBJECTIVE: The study aim was to assess systemic EPA and EPA + DHA exposures and plasma lipid parameters following multiple OM3-CA or IPE doses under low-fat dietary conditions, and dose proportionality after OM3-CA administration...
January 23, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28078530/evaluation-of-the-population-pharmacokinetic-properties-of-lidocaine-and-its-metabolites-after-long-term-multiple-applications-of-a-lidocaine-plaster-in-post-herpetic-neuralgia-patients
#11
Roberta Bursi, Chiara Piana, Joachim Grevel, Dymphy Huntjens, Irmgard Boesl
BACKGROUND AND OBJECTIVES: Lidocaine 5% medicated plaster is the first lidocaine containing product for chronic use. As no previous investigations have been conducted to evaluate the population pharmacokinetics of long-term exposure to lidocaine 5% medicated plasters, further insights into the evaluation of the pharmacokinetic properties of lidocaine and its metabolites were needed for the assessment of its safety. METHODS: The population pharmacokinetic properties of lidocaine and its metabolites were evaluated after multiple applications of lidocaine 5% medicated plasters based on data collected for up to 14...
January 12, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070880/on-the-molecular-basis-underlying-the-metabolism-of-tapentadol-through-sulfation
#12
Ahsan F Bairam, Mohammed I Rasool, Katsuhisa Kurogi, Ming-Cheh Liu
BACKGROUND AND OBJECTIVES: Previous studies reported that tapentadol-sulfate represented one of the major metabolites of tapentadol excreted in urine. The current study aimed to identify the human cytosolic sulfotransferases (SULTs) that is(are) capable of sulfating tapentadol and to examine whether human cells and human organ specimens are capable of sulfating tapentadol. METHODS: Thirteen human SULTs, previously expressed and purified, as well as human organ cytosols, were analyzed for tapentadol-sulfating activity using an established sulfotransferase assay...
January 10, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070879/a-review-of-pharmacogenetics-of-antimalarials-and-associated-clinical-implications
#13
REVIEW
Hazem Elewa, Kyle John Wilby
Genetic variability in drug-metabolizing enzymes and drug transporters is known to influence the pharmacokinetics of many drugs. Antimalarial drugs are a class of agents known to utilize metabolic and elimination pathways prone to genetic variation. This paper aims to review the genetic variants affecting antimalarial medications and discuss their clinical implications. Data were identified for the genes coding for the cytochrome P450 (CYP) enzymes: CYP2C8, CYP2C19, CYP2A6, CYP2D6, CYP2B6, and the P-glycoprotein drug transporter...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28070878/effects-of-caffeic-acid-and-quercetin-on-in-vitro-permeability-metabolism-and-in-vivo-pharmacokinetics-of-melatonin-in-rats-potential-for-herb-drug-interaction
#14
Snehasis Jana, Himanshu Rastogi
BACKGROUND AND OBJECTIVES: Melatonin is a popular dietary supplement and also considered as pharmaceutical product for sleep disorders. Caffeic acid and quercetin are widely distributed in leafy vegetables, fruits, tea extract, and both are used as natural antioxidant. There is an immense concern for health researchers to study the herb/food-drug interactions of melatonin. It is mainly metabolized by CYP1A2 in human so that herbs/foods containing cytochrome P450 (CYP) inhibitors can affect pharmacokinetics of melatonin...
January 9, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28064419/pharmacokinetics-and-pharmacogenetics-of-carbamazepine-in-children
#15
Natasa Djordjevic, Slobodan M Jankovic, Jasmina R Milovanovic
Although carbamazepine is one of the oldest anticonvulsant drugs, it is still heavily utilized for treatment of epilepsy in children. The aim of this article was to review the current knowledge about pharmacokinetics and pharmacogenetics of carbamazepine in children. The literature for this review was systematically searched for in the MEDLINE and SCINDEKS databases. Oral bioavailability of carbamazepine in children is about 75-85%, and it is approximately 75-85% bound to plasma proteins. Apparent volume of distribution is 1...
January 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28064418/novel-antiretroviral-drugs-in-patients-with-renal-impairment-clinical-and-pharmacokinetic-considerations
#16
Dario Cattaneo, Cristina Gervasoni
Highly active antiretroviral therapy (HAART) has dramatically increased the survival of HIV-infected patients from Western countries reducing the incidence of opportunistic infections and AIDS-related malignancies, and improving the patients' quality of life compared with the pre-HAART era. HIV is thus now considered in the West as a chronic disease, with the majority of HIV-infected patients successfully reaching an optimal immune and virological outcome a few months after starting HAART. However, this switch from acute to chronic disease has been accompanied by an increased incidence of chronic kidney disease (CKD), reported in up to 60% of HIV-infected patients...
January 7, 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27220743/methylphenidate-for-treating-adhd-a-naturalistic-clinical-study-of-methylphenidate-blood-concentrations-in-children-and-adults-with-optimized-dosage
#17
Maria D Chermá, Martin Josefsson, Irene Rydberg, Per Woxler, Tomas Trygg, Olle Hollertz, Per A Gustafsson
BACKGROUND: Methylphenidate (MPH), along with behavioral and psychosocial interventions, is the first-line medication to treat attention-deficit hyperactivity disorder (ADHD) in Sweden. The dose of MPH for good symptom control differs between patients. However, studies of MPH concentration measurement in ADHD treatment are limited. OBJECTIVE: To describe blood and oral fluid (OF) concentrations of MPH after administration of medication in patients with well-adjusted MPH treatment for ADHD, and to identify the most suitable matrix for accurate MPH concentration during treatment...
April 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27209586/a-two-period-open-label-single-dose-crossover-study-in-healthy-volunteers-to-evaluate-the-drug-drug-interaction-between-cimetidine-and-inhaled-extrafine-chf-5993
#18
Fabrizia Mariotti, Giorgia Ciurlia, Luca Spaccapelo, Annamaria Muraro, Daniela Acerbi
BACKGROUND AND OBJECTIVES: CHF 5993 is an extrafine 'triple therapy' combination of the long-acting muscarinic antagonist glycopyrronium bromide (GB), the long-acting β2-agonist formoterol fumarate (FF), and the inhaled corticosteroid beclometasone dipropionate (BDP). It is in development for chronic obstructive pulmonary disease and asthma delivered via pressurised metered-dose inhaler. METHODS: This two-period, open-label, crossover study examined the drug-drug interaction of CHF 5993 and cimetidine...
April 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/27180066/pharmacokinetics-and-bioavailability-of-the-gnrh-analogs-in-the-form-of-solution-and-zn-2-suspension-after-single-subcutaneous-injection-in-female-rats
#19
Aleksandra Suszka-Świtek, Florian Ryszka, Barbara Dolińska, Renata Dec, Alojzy Danch, Łukasz Filipczyk, Ryszard Wiaderkiewicz
BACKGROUND AND OBJECTIVES: Although many synthetic gonadoliberin analogs have been developed, only a few of them, including buserelin, were introduced into clinical practice. Dalarelin, which differs from buserelin by just one aminoacid in the position 6 (D-Ala), is not widely used so far. Gonadotropin-releasing hormone (GnRH) analogs are used to treat many different illnesses and are available in different forms like solution for injection, nasal spray, microspheres, etc. Unfortunately, none of the above drug formulations can release the hormones for 24 h...
April 2017: European Journal of Drug Metabolism and Pharmacokinetics
https://www.readbyqxmd.com/read/28101841/influence-of-sex-and-food-on-the-bioavailability-and-the-r-to-s-conversion-of-ketoprofen-stereoisomers-in-humans
#20
LETTER
Pietro Fagiolino, Nikoletta Fotaki, Marta Vázquez
No abstract text is available yet for this article.
February 2017: European Journal of Drug Metabolism and Pharmacokinetics
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